{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T19:44:51Z","timestamp":1760298291957,"version":"3.38.0"},"reference-count":43,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2010,11,9]],"date-time":"2010-11-09T00:00:00Z","timestamp":1289260800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Synapse"],"published-print":{"date-parts":[[2011,6]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>In vitro binding characteristics of the dopamine D<jats:sub>3<\/jats:sub>\/D<jats:sub>2<\/jats:sub>antagonist [<jats:sup>3<\/jats:sup>H]raclopride were compared to the D<jats:sub>3<\/jats:sub>\/D<jats:sub>2<\/jats:sub>agonist [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO in membrane preparations from rat striatum, cerebellum Lobules 9 and 10 (CB L9,10), and other cerebellar regions. In striatum, both radioligands labeled a single binding site. [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO showed higher affinity, though lower<jats:italic>B<\/jats:italic><jats:sub>max<\/jats:sub>, compared with [<jats:sup>3<\/jats:sup>H]raclopride and was sensitive to inhibition by Gpp(NH)p. [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO showed significant specific binding to CB L9,10 membranes with higher affinity compared to striatal membranes. [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO binds to a high\u2010 and a low\u2010affinity binding site in CB L9,10 membranes; the high\u2010affinity site was not Gpp(NH)p\u2010sensitive. [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO did not significantly bind cerebellum left hemisphere membranes. Very low specific binding of [<jats:sup>3<\/jats:sup>H]raclopride was found in CB L9,10. The selective dopamine D<jats:sub>3<\/jats:sub>antagonist SB\u2010277011 did not displace the binding of either ligand to striatal membranes but potently inhibited the binding of [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO in CB L9,10 membranes. The highly selective D<jats:sub>2<\/jats:sub>antagonist SV\u2010156 showed the opposite profile. In vivo experiments were consistent with and supported by in vitro results. In summary, [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO and [<jats:sup>3<\/jats:sup>H]raclopride mainly label dopamine D<jats:sub>2<\/jats:sub>receptors in rat striatum, with [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO labeling a D<jats:inline-graphic xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" xlink:href=\"graphic\/tex2gif-stack-1.gif\" xlink:title=\"urn:x-wiley:08874476:media:SYN20867:tex2gif-stack-1\"\/>population. In vitro and in vivo, [<jats:sup>3<\/jats:sup>H](+)\u2010PHNO labels CB L9,10 dopamine D<jats:sub>3<\/jats:sub>receptors that are apparently in a high affinity state whereas [<jats:sup>3<\/jats:sup>H]raclopride gave only very low signal in this region. The present approaches appear useful for selectively labeling dopamine D<jats:sub>3<\/jats:sub>and D<jats:sub>2<\/jats:sub>receptors in different rat brain regions and offer the possibility to demonstrate D<jats:sub>3<\/jats:sub>versus D<jats:sub>2<\/jats:sub>receptor selectivity of compounds using native rat brain tissue. Synapse, 2011. \u00a9 2010 Wiley\u2010Liss, Inc.<\/jats:p>","DOI":"10.1002\/syn.20867","type":"journal-article","created":{"date-parts":[[2010,10,8]],"date-time":"2010-10-08T19:22:28Z","timestamp":1286565748000},"page":"467-478","source":"Crossref","is-referenced-by-count":28,"title":["In vitro and in vivo comparison of [<sup>3<\/sup>H](+)\u2010PHNO and [<sup>3<\/sup>H]raclopride binding to rat striatum and lobes 9 and 10 of the cerebellum: A method to distinguish dopamine D<sub>3<\/sub>from D<sub>2<\/sub>receptor sites: A method to distinguish dopamine D<sub>3<\/sub>from D<sub>2<\/sub>receptor sites"],"prefix":"10.1002","volume":"65","author":[{"given":"B\u00e9la","family":"Kiss","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ferenc","family":"Horti","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Amrita","family":"Bobok","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2010,11,9]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(94)91052-9"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0893-133X(97)00162-0"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(96)00964-X"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-8993(99)02306-9"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0278-5846(99)00079-2"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(91)91456-B"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(73)90196-2"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/0306-4522(94)00527-C"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.20718"},{"key":"e_1_2_6_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0024-3205(98)00148-9"},{"key":"e_1_2_6_12_1","doi-asserted-by":"crossref","first-page":"417","DOI":"10.1016\/S0022-3565(25)38490-9","article-title":"Expression and pharmacological characterization of the human D3 dopamine receptor","volume":"268","author":"Freedman SB","year":"1994","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_6_13_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.20290"},{"key":"e_1_2_6_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0197-0186(00)00047-4"},{"key":"e_1_2_6_15_1","doi-asserted-by":"publisher","DOI":"10.1254\/jjp.89.309"},{"key":"e_1_2_6_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(85)90778-6"},{"key":"e_1_2_6_17_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00702-007-0009-0"},{"key":"e_1_2_6_18_1","doi-asserted-by":"crossref","first-page":"231","DOI":"10.1016\/S0031-6997(24)01327-9","article-title":"The D3 dopamine receptor: Neurobiology and potential clinical relevance","volume":"49","author":"Levant B","year":"1997","journal-title":"Pharmacol Rev"},{"key":"e_1_2_6_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-8993(98)00529-0"},{"key":"e_1_2_6_20_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.890140112"},{"key":"e_1_2_6_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(95)00160-M"},{"key":"e_1_2_6_22_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(96)00239-0"},{"key":"e_1_2_6_23_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.89.17.8155"},{"key":"e_1_2_6_24_1","doi-asserted-by":"crossref","first-page":"395","DOI":"10.1016\/S0022-3565(25)21227-7","article-title":"Selectivity of (+)\u20104\u2010propyl\u20109\u2010hydroxynaphthoxazine [(+)\u2010PHNO] for dopamine receptors in vitro and in vivo","volume":"233","author":"Martin GE","year":"1985","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_6_25_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.3838821"},{"key":"e_1_2_6_26_1","doi-asserted-by":"publisher","DOI":"10.1038\/npp.2010.50"},{"key":"e_1_2_6_27_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.890170305"},{"key":"e_1_2_6_28_1","first-page":"456.","volume-title":"The rat brain in stereotaxic coordinates","author":"Paxinos G","year":"2007"},{"key":"e_1_2_6_29_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.20771"},{"key":"e_1_2_6_30_1","doi-asserted-by":"publisher","DOI":"10.1002\/syn.20658"},{"key":"e_1_2_6_31_1","doi-asserted-by":"crossref","first-page":"1154","DOI":"10.1016\/S0022-3565(24)39184-0","article-title":"Pharmacological actions of a novel, high\u2010affinity, and selective human dopamine D(3) receptor antagonist. 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